Modified bile acids process for their preparation and their use

Details Modified bile acids process for their preparation and their use Modified bile acids process for their preparation and their use

1995-09-12

1997-06-24

Prior, Kimberly J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

514182, 540 4, 540114, A61K 3158, A61K 31575, C07J 900

Patent

active

056417675

ABSTRACT:
The invention relates to linker-modified bile acid derivatives of the formula I: ##STR1## wherein the radicals X.sup.1, X.sup.2, X.sup.3 and Y and n are as defined in the claims, and to a process for their preparation. The compounds according to the invention are therapeutically active and are thus suitable as drugs, especially as hypolipldemics. The invention further relates to the use of the bile acid derivatives according to the invention as drugs.

REFERENCES:
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patent: 4834919 (1989-05-01), Magni et al.
patent: 5095130 (1992-03-01), Vivat et al.
patent: 5500421 (1996-03-01), Parenti
patent: 5508453 (1996-04-01), Aresio et al.
patent: 5565587 (1996-10-01), Aiosio et al.
Wess, et. et al., "Modified Bile Acids: Preparation of 7.alpha., 12.alpha.-Dihydroxy-3.beta.-and 7.alpha., 12.alpha.-Dihydroxy-3.alpha.(2-Hydropxyethoxy)-5.beta.-Cholanic Acid and Their Biological Activity," Tetrahedron Letters, vol. 33, No. 2, 1992, pp. 195-198.
Kramer et al., "Liver-Specific Drug Tareting by Coupling to Bile Acids", The Journal of Biological Chemistry, 267(26):18598-18604 (1992).
G. Wess et al., "Specific Inhibitors of Ileal Bile Acid Transport", Journal of Medicinal Chemistry, 37(7):873-875 (1994).

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